乌梅抗氧化作用的实验考察

目的:研究乌梅提取物抗氧化作用。方法:通过检测还原力和清除DPPH、ABTS和超氧阴离子自由基的能力,分析和评价乌梅提取物的抗氧化活性。结果:乌梅醇提物对DPPH、ABTS自由基的IC50分别为0.500 mg.mL-1及0.253 mg.mL-1;乌梅水提物对DPPH、ABTS自由基的IC50分别0.510 mg.mL-1及0.500 mg.mL-1;乌梅醇提物还原能力大于乌梅水提物,且乌梅醇提物对超氧阴离子自由基的清除作用显著,其清除作用优于乌梅水提物及对照品BHT。结论:乌梅提取物有不同程度的抗氧化活性,其中以醇提物抗氧化作用最强。     

仙茅苷对自由基的清除作用

目的研究仙茅(Curculigo orchioidesGaertn.)主要成分仙茅苷(curcu ligoside)对羟自由基和超氧阴离子自由基的清除作用。方法分别采用比色法及电子顺磁共振技术(ESR)测定仙茅苷对羟自由基和超氧阴离子自由基的清除效果。结果仙茅苷对羟自由基和超氧阴离子自由基均有良好的清除作用,其清除率略低于茶多酚。结论仙茅苷对自由基具有明显的清除作用,是一种有效的天然抗氧化剂。     

芦荟中芦荟苷清除超氧阴离子自由基的ESR研究

目的　从分子水平探讨芦荟保健美容的作用机制。方法　利用电子自旋共振 (ESR)法,以二甲基亚砜在碱性条件下产生超氧阴离子自由基(O-·2 )体系,检测芦荟中主要有效成分芦荟苷清除O-·2 的能力。结果　芦荟苷具有良好的清除超氧阴离子自由基(O-·2 )的作用,芦荟苷浓度为 0. 26mg/mL时,对O-·2 的清除率达 100%。结论　芦荟的保健美容作用可能与其主要有效成分芦荟苷具有清除超氧阴离子自由基的能力有关。     

仙茅苷对自由基的清除作用

目的研究仙茅(Curculigo orchioides Gaertn.)主要成分仙茅苷(curcu ligoside)对羟自由基和超氧阴离子自由基的清除作用。方法分别采用比色法及电子顺磁共振技术(ESR)测定仙茅苷对羟自由基和超氧阴离子自由基的清除效果。结果仙茅苷对羟自由基和超氧阴离子自由基均有良好的清除作用,其清除率略低于茶多酚。结论仙茅苷对自由基具有明显的清除作用,是一种有效的天然抗氧化剂。     

异莲心碱的体外抗氧化活性

目的研究异莲心碱对氧自由基的清除作用及其对脂质过氧化反应(LPO)的抑制作用。方法羟自由基由Fenton体系产生,超氧阴离子自由基由邻苯三酚自氧化法产生,通过比色法测定LPO的终产物 丙二醛(MDA)的相对含量来反映异莲心碱对LPO的影响。结果异莲心碱对羟自由基和超氧阴离子自由基有较强的清除作用,达到5 0 %清除率所需药物浓度(EC50 )分别为0 .90 ,1.82mg/ml,可抑制小鼠肝匀浆脂质过氧化反应,EC50 为0 .6 7mg/ml。结论异莲心碱对氧自由基有清除作用,对脂质过氧化有抑制作用,其活性与剂量呈正相关     

桂花不同溶剂提取物对氧自由基清除作用的ESR研究

目的研究桂花不同提取物对氧自由基的清除作用。方法利用不同极性溶剂（水、石油醚、乙酸乙酯、正丁醇）浸提桂花粉后得到不同极性的提取物。通过电子自旋共振（ESR）和自旋捕集技术,以1,1-二苯基-2-三硝基苯肼自由基（DPPH）及核黄素光照条件下产生超氧阴离子O2^-自由基体系,检测桂花中各组分清除DPPH自由基及O2^-的能力。结果以维生素C为对照,桂花水提取物、石油醚提取物、乙酸乙酯提取物、正丁醇提取物及维生素C清除DPPH自由基能力IC50分别为59.63,53.93,28.33,38.89,40.93μg·mL^-1;各提取物及维生素C对超氧阴离子O2-自由基清除能力IC50分别为63.37,55.47,30.20,48.36,41.52μg·mL^-1。其中各提取物的乙酸乙酯提取物的DPPH及O2^-清除率最大。结论通过比较各组分对DPPH自由基及超氧阴离子自由基的清除能力,了解桂花中抗氧化成分在各相中的分布情况,并据此进行有目的的分离桂花中的抗氧化成分。     

槲皮素-钼配合物对超氧阴离子和羟自由基的清除作用

目的 探讨槲皮素-钼配合物对超氧阴离子自由基(O2-.)和羟自由基(·OH)的清除作用.方法 分别用改良的邻苯三酚法和水杨酸法测定槲皮素一钼配合物对O2-.和·OH的清除作用,并与槲皮素比较.结果 配合物对O2-.和·OH均有显著的清除作用,对·OH的清除作用优于槲皮素(P＜0.05).结论 槲皮素-钼配合物具有较强的清除自由基作用.     

电子顺磁共振技术研究一枝蒿总黄酮抗氧化作用

目的　探讨一枝蒿总黄酮清除自由基的作用。方法　采用电子顺磁共振技术 (EPR)分别检测一枝蒿总黄酮对超氧阴离子自由基 (O·2 ) ,羟自由基 (·OH)的清除作用。结果　一枝蒿总黄酮对超氧阴离子自由基、羟自由基具有不同程度的清除作用 ,且存在明显的药物浓度—清除效用关系。结论　一枝蒿总黄酮有明显的抗氧化作用     

5,7,4’-三羟基异黄酮基-8-对偶氮苯磺酸的合成及其抗氧化活性研究

目的合成未见文献报道的化合物5,7,4’-三羟基异黄酮基-8-对偶氮苯磺酸,并探讨其抗氧化活性。方法采用IR、1H-NMR、元素分析对其结构进行表征。利用荧光光谱法研究目标物对羟基自由基的清除活性,采用紫外光谱法研究目标物对超氧阴离子自由基和1,1-二苯基-2-苦肼基自由基(DPPH·)的清除活性。结果与结论目标化合物对1,1-二苯基-2-苦肼基自由基、羟基自由基和超氧阴离子自由基都有良好的清除活性,而且对羟基自由基的清除活性远高于对超氧阴离子自由基和1,1-二苯基-2-苦肼基自由基的清除活性。     

红景天中8种成分体外抗氧化作用的比较

目的比较性研究红景天中8种苷及醇类化合物———芦丁苷、红景天苷、异槲皮苷、酪醇、络塞琳、熊果苷、络塞维、肉桂醇红景天的体外抗氧化作用。方法测定8种成分对DPPH自由基、超氧阴离子自由基、一氧化氮自由基、羟自由基的清除能力,以及总抗氧化能力和抑制脂质过氧化反应的能力。结果除清除羟自由基实验外,异槲皮苷和芦丁苷作用明显强于其他化合物,其中在清除DPPH、超氧阴离子能力和抑制脂质过氧化实验中的IC50分别为5.72和10.46,23.63和36.39,10.78和56.49 mg.L-1;而在清除羟自由基实验中,酪醇和红景天苷的作用则强于其他化合物,IC50分别为10.84和18.97 mg.L-1。结论红景天中苷及醇类成分对多种自由基具有清除作用,有良好的综合抗氧化性和开发应用前景。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.